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Amphiphilic polypeptide and preparation method and application thereof

An amphiphilic and reactive system technology, applied in the field of application of amphiphilic polypeptide YIGSRHHHLLLGFLG, protein polypeptide and anticancer drug delivery system, preparation, and new anticancer drug delivery, can solve the problem of poor solubility, poor stability, anti-tumor Drug delivery lacks targeting and other problems, to achieve the effect of improving effect, high stability, and improving drug loading and solubility

Active Publication Date: 2021-01-29
WANNAN MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Aiming at the current problems of lack of targeting, poor solubility and poor stability in the delivery of anticancer drugs, the present invention provides an amphiphilic polypeptide P15 (YIGSRHHHLLLGFLG) and its preparation method, a novel anticancer drug delivery system and its preparation method , the YIGSR sequence in the polypeptide can target and bind 67LR; at the same time, the amphiphilic property of the polypeptide can be used to load anti-tumor drugs, especially hydrophobic anti-tumor drugs, such as paclitaxel, etc., which can form an amphiphilic spherical polymer state with a hydrophobic core and a hydrophilic shell. It not only improves the load rate, but also makes it more stable

Method used

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  • Amphiphilic polypeptide and preparation method and application thereof
  • Amphiphilic polypeptide and preparation method and application thereof
  • Amphiphilic polypeptide and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] MCF-7 cell line has been used to study the research of anticancer activity and PTX activity, utilizes the novel anticancer drug delivery system prepared by the method of the present invention to study the influence of MCF-7 cell line, is divided into three steps altogether:

[0080] Step (1): Preparation of amphiphilic polypeptide YIGSRHHHLLLGFLG

[0081] a. Weigh 1g of 2-cl resin (the degree of substitution of resin drug loading is 0.5), soak it in 20mL of DCM at 20°C for 2min, then wash once with DMF and DCM; use 20mL of DCM as solvent, weigh 0.2g of Fmoc-Asp(Otbu)-OH, reacted with 1mL of DIEA, 1g of 2-cl resin at 20°C for 1.5h, then washed twice with DMF; capped with 20mL of DCM+1mL of methanol+1mLDIEA at 20°C for 30min, and used Wash 3 times with DMF; deprotect with 15mL piperidine at 20°C, react for 15min, then wash 4 times with DMF until ninhydrin is detected as blue;

[0082] b. Add 0.4gY and 0.5g HoBt to the system, add 1mL TBTU as catalyst, 20mLDMF as solvent,...

Embodiment 2

[0099] The preparation of the amphiphilic polypeptide and the novel anticancer drug delivery system by the method of the present invention is divided into two steps:

[0100] Step (1): Preparation of amphiphilic polypeptide YIGSRHHHLLLGFLG

[0101] a. Weigh 1g of 2-cl resin (the degree of substitution of resin drug loading is 0.5), soak it in 20mL of DCM at 20°C for 2min, then wash once with DMF and DCM; use 20mL of DCM as solvent, weigh 0.3g of Fmoc-Asp(Otbu)-OH, react with 1mL of DIEA, 1g of 2-cl resin at 25°C for 2h, then wash twice with DMF; use 20mL of DCM+1mL of methanol+1mLDIEA at 20°C for 45min, wash with DMF Wash 3 times; deprotect with 15mL piperidine at 25°C, react for 15min, then wash 4 times with DMF until ninhydrin is detected as blue;

[0102] b. Add 0.5gY and 0.5g HoBt to the system, add 1mL TBTU as catalyst, 20mLDMF as solvent, react at 20°C for 1h, then wash 3 times until ninhydrin is detected as blue; add 0.9gR, 0.4gG in sequence , 0.5gS, 0.9gH, 0.5gL, 0.5...

Embodiment 3

[0110] The preparation of the amphiphilic polypeptide and the novel anticancer drug delivery system by the method of the present invention is divided into two steps:

[0111] Step (1): Preparation of amphiphilic polypeptide YIGSRHHHLLLGFLG

[0112] a. Weigh 1g of 2-cl resin (the degree of substitution of resin drug loading is 0.5), soak it in 30mL of DCM at 20°C for 2min, then wash once with DMF and DCM; use 30mL of DCM as solvent, weigh 0.4g of Fmoc-Asp(Otbu)-OH, reacted with 1.5mL of DIEA, 1g of 2-cl resin at 20°C for 2.5h, then washed twice with DMF; capped with 30mL of DCM+1mL of methanol+1mLDIEA at 20°C for 30min, Wash 3 times with DMF; deprotect with 20mL piperidine at 20°C, react for 30min, then wash 4 times with DMF until ninhydrin is detected as blue;

[0113] b. Add 0.6gY and 0.6g HoBt to the system, add 1.5mL TBTU as catalyst, 30mLDMF as solvent, react at 20°C for 1.5h, then wash 3 times until ninhydrin is detected as blue; add 0.9gR in turn, 0.4gG, 0.5gS, 0.9gH, ...

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Abstract

The invention belongs to the technical field of pharmacy, and discloses an amphiphilic polypeptide P15 (YIGSRHHHLLLGFLG), and a preparation method and application thereof. The amphiphilic polypeptideis synthesized by a solid-phase synthesis method after optimization of resin, a catalyst and a feeding ratio, and is applied to preparation of an anti-cancer drug delivery system P15-PTX, the preparation method comprises the following steps: mixing and dissolving the amphiphilic polypeptide and paclitaxel (PTX) in water, and then dialyzing the system for multiple times, and finally, carrying out centrifugal treatment on the dialyzed system to remove supernatant. The novel anti-cancer drug delivery system has the advantages of strong targeting effect, good stability, high entrapment rate, few side effects, low toxicity and the like, and can obviously improve the drug effect.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and relates to a protein polypeptide and an anticancer drug delivery system. Specifically, it relates to the amphiphilic polypeptide YIGSRHHHLLLGFLG, its preparation method, and its application in the delivery of novel anticancer drugs. Background technique [0002] All organs in the human body are composed of cells. Orderly cell proliferation and differentiation can meet the needs of the body and maintain good health. However, if the cells continue to divide, no longer under the control of the body, and reproduce indefinitely, these extra large numbers of cells form a tumor. Cells of malignant tumors can invade and destroy adjacent tissues and organs. Also, cancer cells can break out of the tumor and enter the blood or lymphatic system, becoming life-threatening. [0003] At present, many anti-tumor drugs have been developed, and all of them have effective pharmacological activities, but th...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K9/107A61K31/337A61K45/00A61K47/42A61P35/00
CPCC07K7/08A61K9/1075A61K31/337A61K45/00A61K47/42A61P35/00
Inventor 桂琳郑赟潘中武葛飞
Owner WANNAN MEDICAL COLLEGE
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